The applicants of the present invention disclose novel benzophenone derivatives having inhibitory activity upon microtubule formation in Korean Patent No. 10-2006-0094019 (filed on Sep. 27, 2006), Korean Patent No. 10-2007-0083856 (filed on Aug. 21, 2007) claiming the benefit thereof and PCT Application No. PCT/KR2007/004625 (filed on Sep. 21, 2007).
Among the compounds disclosed in PCT/KR2007/004625, 516[{4-(2-aminothiazol-4-yl)-2-(1H-1,2,4-triazol-1-yl)phenyl}(3,4,5-trimethoxyphenyl)methanone] is found to exhibit potent mitosis inhibitory activity and cytotoxicity. From animal test results, it can be confirmed that the toxicity is caused by deposition on organs due to its low solubility.
Accordingly, the inventors of the present invention attempted to develop compounds which exhibit more efficacious pharmaceutical effects and low toxicity via improvement in solubility of benzophenone derivatives, resulting in the present invention. That is, the present invention provides novel benzophenone thiazole compounds, as derivatives of 516[{4-(2-aminothiazol-4-yl)-2-(1H-1,2,4-triazol-1-yl)phenyl}(3,4,5-trimethoxyphenyl)methanone], having efficient mitosis inhibition, superior antitumor activity, and improved solubility and thus considerably decreased toxicity.